Bioactivity and Cell Imaging of Antitumor Fluorescent Agents (Curcumin Derivatives) Coated by Two-Way Embedded...

Area of Science:

• Medicinal Chemistry
• Biotechnology
• Pharmacology

Background:

• Curcumin exhibits broad pharmacological activities for treating diseases like tumors and inflammation.
• Poor solubility and low bioavailability of curcumin limit its therapeutic applications.
• Development of novel curcumin derivatives is crucial for enhanced drug delivery and efficacy.

Purpose of the Study:

• To synthesize novel fluorescent curcumin derivatives by modifying its structure.
• To improve curcumin's properties by forming inclusion complexes with cyclodextrins (α-cyclodextrin and hydroxypropyl β-cyclodextrin).
• To evaluate the photophysical properties and anti-cancer effects of the synthesized compounds.

Main Methods:

• Curcumin structure was modified using boron trifluoride ether for fluorescent labeling.
• Inclusion complexes were formed by embedding modified curcumin into α-cyclodextrin and hydroxypropyl β-cyclodextrin.
• Photophysical properties (emission wavelength) were analyzed.
• Fluorescence imaging was performed on HCT-116 and HeLa cancer cells.
• Cell proliferation toxicity was assessed.

Main Results:

• The synthesized inclusion complexes exhibited excellent photophysical properties with maximum emission wavelengths between 550-565 nm.
• The compounds demonstrated effective fluorescence imaging capabilities in HCT-116 and HeLa cells.
• Both modified curcumin compounds showed significant inhibitory effects on cancer cell proliferation.
• The novel compounds possess great reference value for developing new curcumin dosage forms.

Conclusions:

• Modified curcumin derivatives complexed with cyclodextrins possess enhanced photophysical properties and anti-cancer activity.
• These fluorescent curcumin-cyclodextrin complexes show promise for cancer diagnosis and therapy.
• The study highlights the potential of structural modification and complexation to overcome curcumin's limitations for drug development.